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Inhibitors & Agonists

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Cat. No. Product Name Field of Application Chemical Structure
DC72371 Tiprelestat
Tiprelestat is a potent human neutrophil elastase inhibitor. Tiprelestat has antimicrobial and anti-inflammatory activities. Tiprelestat can be used in the research of inflammation/immune disease.
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DC72370 VM4-037
VM4-037 can be used for the synthesis of VM4-037(18F). VM4-037(18F) is a fluorinated PET imaging agent for carbonic anhydrase IX.
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DC72369 RXPA 380
RXPA 380 is a C-terminal specific angiotensin-converting enzyme (ACE) inhibitor with a Ki of 3 nM. RXPA 380 inhibits C-domain mutants of human recombinant ACE with an IC50 of 2.5 nM.
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DC72368 STL5-T-0057
STL5-T-0057 (compound 68) is an selective ALDH1 B1 inhibitor with an IC50 value of 30 nM. STL5-T-0057 inhibits cell growth of SW480 cells in adherent and spheroid conditions with IC50 values of 2.46 and 0.39 μM, respectively. STL5-T-0057 can be used for the research of cancer.
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DC72366 Farnesyl pyrophosphate
Farnesyl pyrophosphate, a 15-carbon isoprenoid, is a metabolic intermediate of the mevalonate (MVA) pathway. Farnesyl pyrophosphate is a TRPM2 (TRP Channel) agonist, activates TRPM2 opening for ion influx. Farnesyl pyrophosphate is a key branch substrate for cholesterol synthesis, ubiquinones synthesis, protein farnesylation decoration, and geranyl-geranyl pyrophosphate (GGPP) synthesis.
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DC72364 4,9-Anhydrotetrodotoxin
4,9-Anhydrotetrodotoxin is a selective voltage-gated sodium channel (< a href=" " class="link-product" target="_blank">VGSC) inhibitor that blocks Nav1.1 and Nav1.6 in human brain and induces a hyperpolarizing shift in the voltage dependence of inactivated Nav1.6.
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DC72363 β-Bag cell peptide
β-Bag cell peptide is a neuroactive peptide. β-Bag cell peptide elevates cyclic AMP levels in the bag cell neurons. β-Bag cell peptide decreases the amplitudes of the voltage-dependent potassium currents.
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DC72362 TRAM-39
TRAM-39 is a selective blocker of intermediate conductance Ca2+-activated K+ (IKCa) channels. TRAM-39 inhibits KCa3.1 channel with an IC50 value of 60 nM. TRAM-39 can be used for the research of ataxia, epilepsy, memory disorders, schizophrenia and Parkinson’s disease.
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DC72361 MRS4596
MRS4596 is a potent and selective P2X4 receptor antagonist with an IC50 value of 1.38 μM for human P2X4 receptor. MRS4596 has neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4596 can be used in research of ischemic stroke .
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DC72360 MRS4719
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.
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DC72359 PHA-543613 dihydrochloride
PHA-543613 dihydrochloride is a potent, orally active, brain-penetrant and selective α7 nAChR agonist with a Ki value of 8.8 nM. PHA-543613 dihydrochloride displays selectivity for α7-nAChR over α3β4, α1β1γδ, α4β2 and 5-HT3 receptors. PHA-543613 dihydrochloride can be used for the cognitive deficits of Alzheimer's disease and schizophrenia research.
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DC72358 (R)-Olacaftor
(R)-Olacaftor ((R)-VX-440) is a Cystic fibrosis transmembrane conductance regulator (CFTR) modulator. (R)-Olacaftor has good potential for the study of cystic fibrosis (CF).
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DC72357 inS3-54-A18
inS3-54A18 is a potent inhibitor of STAT3 with anti-cancer properties.
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DC72356 GYY4137
GYY4137 is a novel, water-soluble hydrogen sulfide (H2S)–releasing molecule with vasodilator and antihypertensive activity. GYY4137 shows potent anti-hepatocellular carcinoma activity through blocking the STAT3 pathway. GYY4137 also shows anti-inflammatory activity.
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DC72355 STX-0119
STX-0119 is a selective, orally active STAT3 dimerization inhibitor. STX-0119 inhibits STAT3 transcription with an IC50 of 74 μM.
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DC72354 Mal-Pc
Mal-Pc is a versatile molecular photosensitizer designed based phthalocyanine and maleimides. Mal-Pc can react with GSH to deplete GSH and reduce aggregation, thereby improving ROS (Reactive Oxygen Species)-mediated effect of photodynamic therapy (PDT) in cancer cells.
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DC72353 CM-H2DCFDA
CM-H2DCFDA is a derivative of H2DCFDA. CM-H2DCFDA can be used to determine cellular oxidant levels (Ex/Em: 495/530 nm). CM-H2DCFDA is light-sensitive.
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DC72352 TMX-201
TMX-201 is a TLR7 ligand-phospholipid conjugate. TMX-201 shows potent immune stimulatory activity. TMX-201 can be used for breast cancer and melanoma research.
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DC72351 CDN-A
CDN-A is a cyclic di-nucleotide, it can be used to synthesis antibody-drug conjugate (ADC). Cyclic di-nucleotides are potent stimulators of innate and adaptive immune responses. In humans, cyclic di-nucleotide, which are either produced endogenously in response to foreign DNA or by invading bacterial pathogens, trigger the innate immune system by activating the expression of interferon genes.
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DC72350 KTX-955
KTX-955 is a potent IRAK4 degrader with DC50 values of 5 nM and 130 nM for IRAK4 and Ikaros, respectively. KTX-955 can be used to research anticancer.
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DC72348 Selepressin
Selepressin (FE 202158) is a selective vasopressin V1A receptor agonist. Selepressin is a potent vasopressor. Selepressin can be used in the research of septic shock.
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DC72347 TT-232
TT-232 (CAP-232), a somatostatin derivative, is a peptide SSTR1/SSTR4 agonist. TT-232 inhibits cancer cell proliferation and induces apoptosis. TT-232 is also a broad-spectrum anti-inflammatory and analgesic agent.
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DC72346 MRS2279 diammonium
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05.
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DC72345 PIT
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma.
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DC72344 NAQ
NAQ is a potent and selective μ opioid receptor partial agonist, with a Ki of 0.55 nM. NAQ shows selectivity for Mu opioid receptor over the δ receptor (Ki=132.50 nM) and the κ receptor (Ki=26.45 nM). NAQ can be used for the research of opioid withdrawal or dependence.
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DC72343 ZP 120C
ZP 120C is a potent and partial ORL1 receptor agonist. ZP 120C inhibits electrically induced contraction. ZP 120C can be used in the research of hyponatremia/hypokalemia.
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DC72342 MEN 10207
MEN 10207 is a selective NK-2 tachykinin receptor (Neurokinin Receptor) antagonist. MEN 10207 has pA2 values of 5.2, 7.9 and 4.9 in three monoreceptor in vitro assays for NK-1, NK-2 and NK-3 tachykinin receptors, respectively.
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DC72341 Septide
Septide ((Pyr6,Pro9)-Substance P) is a potent NK1 receptor agonist with a Kd value of 0.55 nM.
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DC72340 (S,S)-BMS-984923
(S,S)-BMS-984923 is a less active (S,S)-enantiomer of BMS-984923. (S,S)-BMS-984923 shows an EC50 >1μM for mGluR5 receptor. BMS-984923 is a potent mGluR5 silent allosteric modulator.
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DC72338 DIBA-Cy5
DIBA-Cy5 is a fluorescent DIBA antagonist made up be DIBA-alkyne binding Cyanine5 fluorophores (Cy5) and polyethylene glycol (PEG) biomolecules. DIBA-Cy5 can serve as a fluorescent ligand, suitable for probe attachment through click chemistry. DIBA-Cy5 exerts a high binding affinity to type-2 mAChR (M2R) with the Kd value of 1.80 nM, can directly stain M2R receptors in the sinoatrial node of a mouse heart.
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